Ethyl Acetoacetate → HCID 59376005、化合物

HRID 661487ノート

反応式

HRID 661487 の反応式
N1C2CCCC(=O)C=2C=C1.C(OCC)(=O)CC(C)=O.P([O-])(O)(O)=O.[Na+].O=P12OP3(OP(OP(O3)(O1)=O)(=O)O2)=O.[CH3:40][C:41]1[NH:42][C:43]2[C:44](=[O:55])[CH2:45][CH2:46][CH2:47][C:48]=2[C:49]=1[C:50]([O:52]CC)=[O:51]>>[CH3:40][C:41]1[NH:42][C:43]2[C:44](=[O:55])[CH2:45][CH2:46][CH2:47][C:48]=2[C:49]=1[C:50]([OH:52])=[O:51]

参加物

6

反応物 5

HCID 8868Ethyl AcetoacetateHCID 14812Phosphorus oxide (P4O10)HCID 2802291,5,6,7-Tetrahydro-4H-indol-4-oneHCID 23672064Monosodium phosphateHCID 59376018ethyl 2-methyl-7-oxo-4,5,6,7-tetrahydro-1H-indole-3-carboxylate

生成物 1

HCID 59376005HCID 59376005、化合物

実験手順

In one more aspect, the present invention relates to pyrrolo[b]cyclohexanone, the intermediate of Formula (II), which is synthesized by the route outlined below: 6-amino-5-oxohexanoic acid hydrochloride(S1) and ethyl acetoacetate were refluxed in a.q. sodium dihydrogen phosphate to generate substituted pyrrole(S2). Then the compound S2 was solved in polyphosphoric acid (PPA), P2O5 used as dehydrant, reacted to generate ethyl 2-methyl-7-oxo-4,5,6,7-tetrahydro-1H-indole-3-carboxylate (S3) at 70° C. 2-methyl-7-oxo-4,5,6,7-tetrahydro-1H-indole-3-carboxylic acid (S4) is obtained by the hydrolysis of (S3) in 1 mol/L a.q. LiOH. Finally, S4 is reacted with H—R6 at room temperature for 24 hours in DMF to give pyrrolo[b]cyclohexanone of Formula (II) by using a condensation reagent.

後処理

  1. temperaturewere refluxed in a.q
  2. customreacted
  3. customat 70° C

出典と根拠

ORDレコード
ord-30cdfd34733a40c6b35131191a3d4dc2
出典データセット
uspto-grants-2011_12
特許番号
US08084621B2

反応ノート

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